Chitosan–xanthan gum microparticle-based oral tablet for colon-targeted and sustained delivery of quercetin

Caddeo, Carla; Nácher, Amparo; Dı́ez-Sales, Octavio; Merino-Sanjuán, Matilde; Fadda, Anna Maria; Manconi, Maria

doi:10.3109/02652048.2014.913726

Cited by 77 publications

(46 citation statements)

References 23 publications

(24 reference statements)

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“…Although chitosan-based or xanthan gum-based delivery systems are not approved by FDA for intravenous injection, they could be administrated intratumorally, orally or by transdermal route. [11][12][13] Both of these polymers are widely reported for development of various drug delivery systems, in particular chitosan nanoparticles for melanoma treatment. 14,15 Natural compounds with antitumor properties are of great interest, since they are rather cheap and non-toxic for normal cells.…”

Section: Introductionmentioning

confidence: 99%

Ultrasonically Assisted Polysaccharide Microcontainers for Delivery of Lipophilic Antitumor Drugs: Preparation and in Vitro Evaluation

Akasov

Bоrodinа

Zaytseva

et al. 2015

ACS Appl. Mater. Interfaces

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High toxicity, poor selectivity, and severe side effects are major drawbacks of anticancer drugs. Various drug delivery systems could be proposed to overcome these limitations. The aim of this study was to fabricate polysaccharide microcontainers (MCs) loaded with thymoquinone (TQ) by a one-step ultrasonication technique and to study their cellular uptake and cytotoxicity in vitro. Two MC fractions with a mean size of 500 nm (MC-0.5) and 2 μM (MC-2) were prepared and characterized. Uptake of the MCs by mouse melanoma M-3 cells was evaluated in both 2D (monolayer culture) and 3D (multicellular tumor spheroids) models by confocal microscopy, flow cytometry, and fluorimetry. The higher cytotoxicity of the TQ-MC-0.5 sample than the TQ-MC-2 fraction was in good correlation with higher MC-0.5 accumulation in the cells. The MC-0.5 beads were more promising than the MC-2 particles because of a higher cellular uptake in both 2D and 3D models, an enhanced antitumor effect, and a lower nonspecific toxicity.

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Section: Introductionmentioning

confidence: 99%

Ultrasonically Assisted Polysaccharide Microcontainers for Delivery of Lipophilic Antitumor Drugs: Preparation and in Vitro Evaluation

Akasov

Bоrodinа

Zaytseva

et al. 2015

ACS Appl. Mater. Interfaces

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“…Interactions between Ch amino groups and X carboxyl groups also result in the formation of PECs, which are already used for the immobilization of enzymes and probiotic bacteria and to produce microspheres, tablets, microcapsules, membranes, controlled release systems, and scaffolds for regenerative medicine applications …”

Section: Introductionmentioning

confidence: 99%

Polysaccharide‐based membranes loaded with erythromycin for application as wound dressings

Souza

Moraes

2016

J of Applied Polymer Sci

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In this study, the antibiotic erythromycin (Ery) was incorporated into chitosan (Ch)-alginate (A) and Ch-xanthan (X) membranes with the aim of using them as bioactive wound dressings. Drug incorporation was performed by direct addition (DA) to the polysaccharide mixture and by membrane impregnation in solution (IS). A higher incorporation efficiency was obtained for DA, but higher amounts of drug were loaded into membranes by the IS method (maxima % 2.1 and 0.7 g/g for Ch-X and Ch-A, respectively) because the initial concentration of drug could be higher than that in the DA method. Ery release in phosphate-buffered saline was slow, reaching about 12 and 32 mg of drug/g of membrane in 60 h for Ch-X and 4 and 16 mg/g for Ch-A by the DA and IS methods, respectively. With formulations prepared with IS, the required therapeutic dosage was reached within 60 h, whereas for those incorporating the drug by DA, prolonged use would be required. Both membrane types behaved as drug reservoirs, providing continuous antibiotic release to the wound site. Formulations with higher drug contents showed effective antibacterial activity against two species of bacteria commonly found in skin lesions, Staphylococcus aureus and Pseudomonas aeruginosa, and were thus potentially capable of protecting the wound site from bacterial attack.Erythromycin (Ery) is a medium-spectrum antibiotic of the macrolide family and is produced by Streptomyces erythreus. 6 Susceptible microorganisms include aerobic Gram-positive bacteria, Gram-negative cocci, spirochetes, actinomycetes, rickettsia, Chlamydia trachomatis, Mycoplasma pneumoniae, Legionella pneumophila, nontuberculous mycobacteria, and some anaerobic bacteria. 7 This antibiotic consists of a 13-carbon ring with two sugars attached by glycosidic linkages 8,9 (Figure 1) and has a molecular weight of 733.9 Da. It is slightly soluble in water and very soluble in organic solvents such as ethanol 10 ; it is useful in the therapy of pneumonia, diphtheria, whooping cough, urethritis, and erythrasma and acne treatments. 7 For topical administration, the common dosage is 20 mg/g of vehicle. 11The incorporation of Ery into wound dressings is of interest if prolonged protection and drug delivery are simultaneously desired, mostly for extensive and painful lesions of difficult manipulation. These systems show improved therapy efficiency by means of an appropriate release profile; this leads to drug availability at the wound site for long periods and, thereby, reduces the need for repeated administrations. 12The main purpose of using a wound dressing is to provide a suitable environment at the wound site so that healing is fast

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“…Cholesterol exhibited several sharp crystal reflections [21], TPP was in the monoclinic crystalline phase C2/c (a=16.0, b=5.24, c=11.25 Å, β=93°) [22], and quercetin revealed its anhydrous crystalline form, with multiple sharp peaks of different intensities between 8° and 32° 2θ [23]. Chitosan exhibited two major peaks at around 13° and 19° 2θ, the first one showing stronger intensity, which correspond to the α and β crystal forms and represent the typical fingerprints of the semi-crystalline polymer [13,24].…”

Section: X-ray Diffraction and Dsc Analysesmentioning

confidence: 99%

Cross-linked chitosan/liposome hybrid system for the intestinal delivery of quercetin

Caddeo

Dı́ez-Sales

Pons³

et al. 2016

Journal of Colloid and Interface Science

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109

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1Quercetin is a flavonoid with antioxidant/anti-inflammatory properties, poorly absorbed when 2 administered orally. To increase its bioavailability and optimize its release in the intestine, a hybrid Scattering. 9The release of quercetin in simulated gastric and intestinal pH was investigated, the results showing 10 that the system provided resistance to acidic conditions, and promoted the release in alkaline pH, 11mimicking the intestinal environment. 12The proposed hybrid system represents a promising combination of nanovesicles and chitosan for

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Chitosan–xanthan gum microparticle-based oral tablet for colon-targeted and sustained delivery of quercetin

Abstract: Microparticle tablets represent a promising dosage form for QUE delivery to the colon in the oral therapy of inflammatory-based disorders.

Cited by 77 publications

References 23 publications

Ultrasonically Assisted Polysaccharide Microcontainers for Delivery of Lipophilic Antitumor Drugs: Preparation and in Vitro Evaluation

Ultrasonically Assisted Polysaccharide Microcontainers for Delivery of Lipophilic Antitumor Drugs: Preparation and in Vitro Evaluation

Polysaccharide‐based membranes loaded with erythromycin for application as wound dressings

Cross-linked chitosan/liposome hybrid system for the intestinal delivery of quercetin

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